Lugdunomycin: a novel antibiotic with a new structural scaffold

Scientists at Leiden University's Institute of Biology have found a novel compound which was named lugdunomycin, isolated from a Streptomyces strain.

They identified that it has a unique chemical scaffold and was shown to have antimicrobial activity against the Gram-positive bacterium Bacillus subtilis. The chemical structure has been completely elucidated. Currently, the scientists are seeking partnerships for the next stage of development.

The antibiotics market (over 40 billion USD) is hampered by the lack of new (approved) compounds to answer the growth of antibiotic resistance that poses an increasing threat to treat bacterial infections. Only two completely new classes of antibiotics have been introduced over the past 30 years: the oxazolidinone linezolid (Zyvox; Pfizer) in 2000 and the cyclic lipopeptide daptomycin (Cubicin; Cubist) in 2003. Novel antibiotics are urgently needed and a novel chemical scaffold has not been found for a number of years.

The novelty in the chemical construction of lugdunomycin is the polycyclic parallelism. From the perspective of the biosynthesis pathway, lugdunomycin potentially has close relationship to angucycline-type antibiotics. With regard to the bioactivity, lugdunomycin showed antimicrobial inhibition effect against bacterium Bacillus subtilis.

Key benefits

Unique chemical structure: unique mechanism of action?

Novel target: identification of additional compounds?

Applications

Treatment of patients suffering from bacterial infections that cannot be resolved by currently available antibiotics due to (multiple) resistance problems.

Development stage

The chemical structure has been elucidated.

Further development involves the biosynthetic pathway and bioactivity of the compound, identification of the gene cluster and improving the yield.

Luris reference number

INV-081.081

Patent status

​A priority patent application has been filed.

Data available on request

Non-confidential and confidential presentations are available upon request.